WO2003081210A3 - Identification of kinase inhibitors - Google Patents

Identification of kinase inhibitors Download PDF

Info

Publication number
WO2003081210A3
WO2003081210A3 PCT/US2003/008725 US0308725W WO03081210A3 WO 2003081210 A3 WO2003081210 A3 WO 2003081210A3 US 0308725 W US0308725 W US 0308725W WO 03081210 A3 WO03081210 A3 WO 03081210A3
Authority
WO
WIPO (PCT)
Prior art keywords
identification
protein kinase
inhibitors
kinase inhibitors
inactive conformation
Prior art date
Application number
PCT/US2003/008725
Other languages
French (fr)
Other versions
WO2003081210A2 (en
Inventor
John C Prescott
Andrew Braisted
Original Assignee
Sunesis Pharmaceuticals Inc
John C Prescott
Andrew Braisted
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sunesis Pharmaceuticals Inc, John C Prescott, Andrew Braisted filed Critical Sunesis Pharmaceuticals Inc
Priority to CA002478981A priority Critical patent/CA2478981A1/en
Priority to AU2003228345A priority patent/AU2003228345B2/en
Priority to EP03726092A priority patent/EP1579186A4/en
Priority to JP2003578895A priority patent/JP2005534286A/en
Publication of WO2003081210A2 publication Critical patent/WO2003081210A2/en
Publication of WO2003081210A3 publication Critical patent/WO2003081210A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C40—COMBINATORIAL TECHNOLOGY
    • C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B30/00—Methods of screening libraries
    • C40B30/04—Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/48—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase
    • C12Q1/485—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving transferase involving kinase
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Analytical Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Medicinal Chemistry (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Peptides Or Proteins (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The invention concerns the identification of protein kinase inhibitors that preferentially bind to the inactive conformation of a target protein kinase. The inhibitors are identified by locking the target protein kinase in an inactive conformation, and using a covalent tethering approach to identify inhibitors preferentially targeting the inactive conformation.
PCT/US2003/008725 2002-03-21 2003-03-20 Identification of kinase inhibitors WO2003081210A2 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
CA002478981A CA2478981A1 (en) 2002-03-21 2003-03-20 Identification of kinase inhibitors
AU2003228345A AU2003228345B2 (en) 2002-03-21 2003-03-20 Identification of kinase inhibitors
EP03726092A EP1579186A4 (en) 2002-03-21 2003-03-20 Identification of kinase inhibitors
JP2003578895A JP2005534286A (en) 2002-03-21 2003-03-20 Identification of kinase inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US36689202P 2002-03-21 2002-03-21
US60/366,892 2002-03-21

Publications (2)

Publication Number Publication Date
WO2003081210A2 WO2003081210A2 (en) 2003-10-02
WO2003081210A3 true WO2003081210A3 (en) 2007-07-26

Family

ID=28454825

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2003/008725 WO2003081210A2 (en) 2002-03-21 2003-03-20 Identification of kinase inhibitors

Country Status (6)

Country Link
US (1) US7202033B2 (en)
EP (1) EP1579186A4 (en)
JP (1) JP2005534286A (en)
AU (1) AU2003228345B2 (en)
CA (1) CA2478981A1 (en)
WO (1) WO2003081210A2 (en)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8097408B2 (en) 2004-10-15 2012-01-17 Galapagos Bv Molecular targets and compounds, and methods to identify the same, useful in the treatment of joint degenerative and inflammatory diseases
US9556426B2 (en) 2009-09-16 2017-01-31 Celgene Avilomics Research, Inc. Protein kinase conjugates and inhibitors
US9562049B2 (en) 2012-12-21 2017-02-07 Medimmune Limited Pyrrolobenzodiazepines and conjugates thereof
US9567340B2 (en) 2012-12-21 2017-02-14 Medimmune Limited Unsymmetrical pyrrolobenzodiazepines-dimers for use in the treatment of proliferative and autoimmune diseases

Families Citing this family (111)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6998233B2 (en) * 1998-06-26 2006-02-14 Sunesis Pharmaceuticals, Inc. Methods for ligand discovery
US6919178B2 (en) * 2000-11-21 2005-07-19 Sunesis Pharmaceuticals, Inc. Extended tethering approach for rapid identification of ligands
US20050084905A1 (en) * 2002-03-21 2005-04-21 Prescott John C. Identification of kinase inhibitors
US20050276812A1 (en) 2004-06-01 2005-12-15 Genentech, Inc. Antibody-drug conjugates and methods
EP1567860A4 (en) * 2002-11-05 2006-05-10 Univ California Methods and materials for examining pathways associated with glioblastoma progression
WO2005034840A2 (en) * 2003-09-17 2005-04-21 Sunesis Pharmaceuticals, Inc. Identification of kinase inhibitors
WO2005035746A2 (en) * 2003-10-02 2005-04-21 Xantos Biomedicine Ag Medical use of tbk-1 or of inhibitors thereof
CN1938046B (en) 2003-11-06 2014-03-19 西雅图基因公司 Monomethylvaline compounds capable of conjugation to ligands
WO2005083441A2 (en) * 2004-02-26 2005-09-09 Bayer Healthcare Ag Diagnostic and therapeutics for diseases associated with proto-oncogene tyrosine-protein kinase (fyn)
WO2006029337A2 (en) * 2004-09-09 2006-03-16 Fox Chase Cancer Center Methods for screening for inhibitors of autoinhibited proteins
DK1791565T3 (en) 2004-09-23 2016-08-01 Genentech Inc Cysteingensplejsede antibodies and conjugates
US20100111856A1 (en) 2004-09-23 2010-05-06 Herman Gill Zirconium-radiolabeled, cysteine engineered antibody conjugates
US8673268B2 (en) 2004-10-15 2014-03-18 Galapagos N.V. Molecular targets and compounds, and methods to identify the same, useful in the treatment of joint degenerative and inflammatory diseases
US20060094682A1 (en) * 2004-10-29 2006-05-04 Odyssey Thera, Inc. Kinase inhibitors for the treatment of diabetes and obesity
ATE477333T1 (en) * 2004-12-16 2010-08-15 Sanofi Aventis Deutschland HIGH-THROUGHPUT ELISA (ENZYME-LINKED IMMUNO ABSORBENT ASSAY) FOR DETERMINING RHO-KINASE (ROK) ACTIVITY
CA2606477C (en) * 2005-04-27 2013-05-28 Siemens Medical Solutions Usa, Inc. In situ click chemistry method for screening high affinity molecular imaging probes
EP2059529A2 (en) * 2006-08-22 2009-05-20 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Screening method for gpcr ligands
ES2403546T3 (en) * 2006-11-03 2013-05-20 Pharmacyclics, Inc. Bruton tyrosine kinase activity probe and method of use
WO2008130921A1 (en) * 2007-04-16 2008-10-30 Modgene, Llc Methods and compositions for diagnosis and treatment of depression and anxiety
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
MX357627B (en) 2008-06-27 2018-07-17 Avila Therapeutics Inc Heteroaryl compounds and uses thereof.
ES2449396T3 (en) 2008-07-22 2014-03-19 Trustees Of Dartmouth College Monocyclic cyanoenones and methods of use thereof
US20100185419A1 (en) * 2008-09-05 2010-07-22 Avila Therapeutics, Inc. Algorithm for designing irreversible inhibitors
JP5918693B2 (en) 2009-05-05 2016-05-18 ダナ ファーバー キャンサー インスティテュート インコーポレイテッド EGFR inhibitor and disease treatment method
US8728763B2 (en) 2009-08-11 2014-05-20 Response Genetics Methods, primers, probes and kits useful for the detection of BRAF mutations
US8470980B2 (en) 2009-09-09 2013-06-25 Centrose, Llc Extracellular targeted drug conjugates
RU2012132473A (en) 2009-12-30 2014-02-10 Селджин Авиломикс,Инк LIGAND-DIRECTED COVALENT PROTEIN MODIFICATION
MA34277B1 (en) 2010-04-15 2013-06-01 Spirogen Developments Sarl PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF
US9000130B2 (en) 2010-06-08 2015-04-07 Genentech, Inc. Cysteine engineered antibodies and conjugates
CN103096716B (en) 2010-08-10 2016-03-02 西建阿维拉米斯研究公司 The benzene sulfonate of BTK inhibitor
JP5957460B2 (en) 2010-11-01 2016-07-27 セルジーン アヴィロミクス リサーチ， インコーポレイテッド Heterocyclic compounds or uses thereof
WO2012061303A1 (en) 2010-11-01 2012-05-10 Avila Therapeutics, Inc. Heteroaryl compounds and uses thereof
WO2012064706A1 (en) 2010-11-10 2012-05-18 Avila Therapeutics, Inc. Mutant-selective egfr inhibitors and uses thereof
WO2012074757A1 (en) 2010-11-17 2012-06-07 Genentech, Inc. Alaninyl maytansinol antibody conjugates
US8513436B2 (en) 2010-12-17 2013-08-20 Reata Pharmaceuticals, Inc. Pyrazolyl and pyrimidinyl tricyclic enones as antioxidant inflammation modulators
RU2638806C2 (en) 2011-05-12 2017-12-15 Дженентек, Инк. Lc-ms/ms method for multiple reactions monitoring to identify therapeutic antibodies in animal species using framework signature peptides
EP2710119A4 (en) * 2011-05-17 2015-02-18 Cleave Biosciences Inc Compositions and methods for jamm protein inhibition
EA026827B1 (en) 2011-10-14 2017-05-31 Медимьюн Лимитед Pyrrolobenzodiazepines and conjugates thereof
EP2770830A4 (en) 2011-10-28 2015-05-27 Celgene Avilomics Res Inc Methods of treating a bruton's tyrosine kinase disease or disorder
WO2013130093A1 (en) 2012-03-02 2013-09-06 Genentech, Inc. Biomarkers for treatment with anti-tubulin chemotherapeutic compounds
MY185243A (en) 2012-03-15 2021-04-30 Celgene Car Llc Salts of an epidermal growth factor receptor kinase inhibitor
EP2825041B1 (en) 2012-03-15 2021-04-21 Celgene CAR LLC Solid forms of an epidermal growth factor receptor kinase inhibitor
WO2014018567A1 (en) 2012-07-24 2014-01-30 Pharmacyclics, Inc. Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk)
KR101995621B1 (en) 2012-10-12 2019-07-03 에이디씨 테라퓨틱스 에스에이 Pyrrolobenzodiazepine-anti-cd22 antibody conjugates
HUE039329T2 (en) 2012-10-12 2018-12-28 Adc Therapeutics Sa Pyrrolobenzodiazepine-antibody conjugates
US10695433B2 (en) 2012-10-12 2020-06-30 Medimmune Limited Pyrrolobenzodiazepine-antibody conjugates
SI2766048T1 (en) 2012-10-12 2015-03-31 Spirogen Sarl Pyrrolobenzodiazepines and conjugates thereof
PT2906298T (en) 2012-10-12 2018-12-28 Medimmune Ltd Pyrrolobenzodiazepine-antibody conjugates
US10736903B2 (en) 2012-10-12 2020-08-11 Medimmune Limited Pyrrolobenzodiazepine-anti-PSMA antibody conjugates
US10751346B2 (en) 2012-10-12 2020-08-25 Medimmune Limited Pyrrolobenzodiazepine—anti-PSMA antibody conjugates
WO2014066506A2 (en) * 2012-10-23 2014-05-01 Cleave Biosciences, Inc. Compositions and methods for jamm protein inhibition
US9126950B2 (en) 2012-12-21 2015-09-08 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
CA2900012A1 (en) 2013-02-08 2014-08-14 Celgene Avilomics Research, Inc. Erk inhibitors and uses thereof
NZ712035A (en) 2013-03-13 2019-06-28 Medimmune Ltd Pyrrolobenzodiazepines and conjugates thereof
BR112015021965B1 (en) 2013-03-13 2022-05-03 Medimmune Limited Pyrrolobenzodiazepine conjugates and compounds, pharmaceutical composition, use thereof for the treatment of a proliferative disease and method of synthesis of said compounds
CA2901941C (en) 2013-03-13 2020-04-07 Spirogen Sarl Pyrrolobenzodiazepines and conjugates thereof
US10442836B2 (en) 2013-08-12 2019-10-15 Genentech, Inc. 1-(chloromethyl)-2,3-dihydro-1H-benzo[E]indole dimer antibody-drug conjugate compounds, and methods of use and treatment
US9492471B2 (en) 2013-08-27 2016-11-15 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase
WO2015052532A1 (en) 2013-10-11 2015-04-16 Spirogen Sàrl Pyrrolobenzodiazepine-antibody conjugates
GB201317982D0 (en) 2013-10-11 2013-11-27 Spirogen Sarl Pyrrolobenzodiazepines and conjugates thereof
US9950078B2 (en) 2013-10-11 2018-04-24 Medimmune Limited Pyrrolobenzodiazepine-antibody conjugates
US9956299B2 (en) 2013-10-11 2018-05-01 Medimmune Limited Pyrrolobenzodiazepine—antibody conjugates
PE20161394A1 (en) 2013-12-16 2017-01-06 Genentech Inc PEPTIDOMIMETIC COMPOUNDS AND THEIR ANTIBODY-DRUG CONJUGATES
JP6671292B2 (en) 2013-12-16 2020-03-25 ジェネンテック， インコーポレイテッド Peptidomimetic compounds and antibody-drug conjugates thereof
CN105828840B (en) 2013-12-16 2020-08-04 基因泰克公司 1- (chloromethyl) -2, 3-dihydro-1H-benzo [ e ] indole dimer antibody-drug conjugate compounds and methods of use and treatment
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
ES2741785T3 (en) 2014-08-13 2020-02-12 Celgene Car Llc Forms and compositions of an ERK inhibitor
WO2016037644A1 (en) 2014-09-10 2016-03-17 Medimmune Limited Pyrrolobenzodiazepines and conjugates thereof
KR20170052600A (en) 2014-09-12 2017-05-12 제넨테크, 인크. Cysteine engineered antibodies and conjugates
GB201416112D0 (en) 2014-09-12 2014-10-29 Medimmune Ltd Pyrrolobenzodiazepines and conjugates thereof
JP6622293B2 (en) 2014-09-12 2019-12-18 ジェネンテック， インコーポレイテッド Anthracycline disulfide intermediates, antibody-drug conjugates, and methods
EA201790359A1 (en) 2014-09-17 2017-08-31 Дженентек Инк. Pyrrolobenzodiazepines and their conjugates associated with disulfide binding to antibodies
BR112017011111A2 (en) 2014-11-25 2017-12-26 Adc Therapeutics Sa pyrrolobenzodiazepine-antibody conjugates
CN107206101B (en) 2014-12-03 2021-06-25 基因泰克公司 Quaternary ammonium compounds and antibody-drug conjugates thereof
GB201506411D0 (en) 2015-04-15 2015-05-27 Bergenbio As Humanized anti-axl antibodies
GB201506402D0 (en) 2015-04-15 2015-05-27 Berkel Patricius H C Van And Howard Philip W Site-specific antibody-drug conjugates
MA43345A (en) 2015-10-02 2018-08-08 Hoffmann La Roche PYRROLOBENZODIAZEPINE ANTIBODY-DRUG CONJUGATES AND METHODS OF USE
CA3000584A1 (en) * 2015-10-02 2017-04-27 Tgr Biosciences Pty Ltd. Analyte detection with multiple substrates
MA43354A (en) 2015-10-16 2018-08-22 Genentech Inc CONJUGATE DRUG CONJUGATES WITH CLOUDY DISULPHIDE
MA45326A (en) 2015-10-20 2018-08-29 Genentech Inc CALICHEAMICIN-ANTIBODY-DRUG CONJUGATES AND METHODS OF USE
US10047058B2 (en) * 2015-12-18 2018-08-14 University Of Southern California Compounds and methods for inhibiting vacuolar ATPase
GB201601431D0 (en) 2016-01-26 2016-03-09 Medimmune Ltd Pyrrolobenzodiazepines
GB201602356D0 (en) 2016-02-10 2016-03-23 Medimmune Ltd Pyrrolobenzodiazepine Conjugates
GB201602359D0 (en) 2016-02-10 2016-03-23 Medimmune Ltd Pyrrolobenzodiazepine Conjugates
WO2017165734A1 (en) 2016-03-25 2017-09-28 Genentech, Inc. Multiplexed total antibody and antibody-conjugated drug quantification assay
GB201607478D0 (en) 2016-04-29 2016-06-15 Medimmune Ltd Pyrrolobenzodiazepine Conjugates
ES2858151T3 (en) 2016-05-20 2021-09-29 Hoffmann La Roche PROTAC-Antibody Conjugates and Procedures for Use
EP3465221B1 (en) 2016-05-27 2020-07-22 H. Hoffnabb-La Roche Ag Bioanalytical method for the characterization of site-specific antibody-drug conjugates
US10639378B2 (en) 2016-06-06 2020-05-05 Genentech, Inc. Silvestrol antibody-drug conjugates and methods of use
CN109689111B (en) 2016-08-11 2024-04-05 基因泰克公司 Pyrrolobenzodiazepine prodrugs and antibody conjugates thereof
CN110139674B (en) 2016-10-05 2023-05-16 豪夫迈·罗氏有限公司 Method for preparing antibody drug conjugates
GB201617466D0 (en) 2016-10-14 2016-11-30 Medimmune Ltd Pyrrolobenzodiazepine conjugates
GB201702031D0 (en) 2017-02-08 2017-03-22 Medlmmune Ltd Pyrrolobenzodiazepine-antibody conjugates
BR112019016373B1 (en) 2017-02-08 2022-01-25 Medimmune Limited Antibody-drug conjugate that binds to axl, composition and pharmaceutical composition comprising the same and therapeutic use of said conjugate
PT3612537T (en) 2017-04-18 2022-08-29 Medimmune Ltd Pyrrolobenzodiazepine conjugates
JP7408396B2 (en) 2017-04-20 2024-01-05 アーデーセー セラピューティクス ソシエテ アノニム combination therapy
AU2018285562B2 (en) 2017-06-14 2024-01-18 Adc Therapeutics Sa Dosage regimes for the administration of an anti-CD19 ADC
EA039276B1 (en) 2017-08-18 2021-12-27 Медимьюн Лимитед Pyrrolobenzodiazepine conjugates
IL302943A (en) 2017-09-20 2023-07-01 Ph Pharma Co Ltd Thailanstatin analogs
GB201803342D0 (en) 2018-03-01 2018-04-18 Medimmune Ltd Methods
GB201806022D0 (en) 2018-04-12 2018-05-30 Medimmune Ltd Pyrrolobenzodiazepines and conjugates thereof
WO2020047475A1 (en) * 2018-08-30 2020-03-05 The Uab Research Foundation Drug screening for fgf23-fgfr4 inhibitors
GB201814281D0 (en) 2018-09-03 2018-10-17 Femtogenix Ltd Cytotoxic agents
WO2020086858A1 (en) 2018-10-24 2020-04-30 Genentech, Inc. Conjugated chemical inducers of degradation and methods of use
EP3894427A1 (en) 2018-12-10 2021-10-20 Genentech, Inc. Photocrosslinking peptides for site specific conjugation to fc-containing proteins
GB201901197D0 (en) 2019-01-29 2019-03-20 Femtogenix Ltd G-A Crosslinking cytotoxic agents
GB2583741B (en) 2019-05-08 2022-03-16 Univ Newcastle Kinase screening assays
WO2021209039A1 (en) * 2020-04-17 2021-10-21 北京赛特明强医药科技有限公司 Quinazoline compound, preparation method therefor and application thereof
GB2597532A (en) 2020-07-28 2022-02-02 Femtogenix Ltd Cytotoxic compounds
CN113061593B (en) * 2021-04-02 2023-11-10 洛阳华荣生物技术有限公司 L-malate dehydrogenase mutant and application thereof

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7083983B2 (en) * 1996-07-05 2006-08-01 Cancer Research Campaign Technology Limited Inhibitors of the interaction between P53 and MDM2
US6919178B2 (en) * 2000-11-21 2005-07-19 Sunesis Pharmaceuticals, Inc. Extended tethering approach for rapid identification of ligands
US6335155B1 (en) * 1998-06-26 2002-01-01 Sunesis Pharmaceuticals, Inc. Methods for rapidly identifying small organic molecule ligands for binding to biological target molecules
AU2573102A (en) 2000-11-21 2002-06-03 Sunesis Pharmaceuticals Inc An extended tethering approach for rapid identification of ligands
IL159900A0 (en) 2001-08-07 2004-06-20 Sunesis Pharmaceuticals Inc Cysteine mutants and methods for detecting ligand binding to biological molecules
NZ530811A (en) 2001-08-07 2005-07-29 Sunesis Pharmaceuticals Inc Disulfide and thiosulfonate ligands and libraries comprising these ligands
IL161409A0 (en) 2001-11-21 2004-09-27 Sunesis Pharmaceuticals Inc Methods for ligand discovery
JP2006523307A (en) * 2003-03-21 2006-10-12 シェーリング　コーポレイション Method for screening a target ligand

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
ERLANSON D.A. ET AL.: "Site-directed ligand discovery", PROC. NATL. ACAD. SCI. U.S.A., vol. 97, no. 17, 15 August 2000 (2000-08-15), pages 9367 - 9372, XP002199107 *
SCHINDLER T. ET AL.: "Structural mechanism for STI-571 inhibition of Abelson tyrosine kinase", SCIENCE, vol. 289, no. 5486, 15 September 2000 (2000-09-15), pages 1938 - 1942, XP002229886 *
SHARMA P. ET AL.: "Identification of Substrate Binding Site of Cyclin-Dependent Kinase 5", J. BIOL. CHEM., vol. 274, no. 14, 2 April 1999 (1999-04-02), pages 9600 - 9606, XP003015671 *
TARRICONE C. ET AL.: "Structure and Regulation of the CDK5-p25nck5a Complex", MOL. CELL, vol. 8, no. 3, September 2001 (2001-09-01), pages 657 - 669, XP003015670 *
WILLIAMS J.C. ET AL.: "Insights into Src kinase functions: structural comparisons", TRENDS BIOCHEM. SCI., vol. 23, no. 5, May 1998 (1998-05-01), pages 179 - 184, XP004118518 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8097408B2 (en) 2004-10-15 2012-01-17 Galapagos Bv Molecular targets and compounds, and methods to identify the same, useful in the treatment of joint degenerative and inflammatory diseases
US9556426B2 (en) 2009-09-16 2017-01-31 Celgene Avilomics Research, Inc. Protein kinase conjugates and inhibitors
US9562049B2 (en) 2012-12-21 2017-02-07 Medimmune Limited Pyrrolobenzodiazepines and conjugates thereof
US9567340B2 (en) 2012-12-21 2017-02-14 Medimmune Limited Unsymmetrical pyrrolobenzodiazepines-dimers for use in the treatment of proliferative and autoimmune diseases

Also Published As

Publication number Publication date
US7202033B2 (en) 2007-04-10
AU2003228345B2 (en) 2009-02-05
US20030232391A1 (en) 2003-12-18
EP1579186A2 (en) 2005-09-28
EP1579186A4 (en) 2008-10-08
JP2005534286A (en) 2005-11-17
CA2478981A1 (en) 2003-10-02
AU2003228345A1 (en) 2003-10-08
WO2003081210A2 (en) 2003-10-02

Similar Documents

Publication Publication Date Title
WO2003081210A3 (en) Identification of kinase inhibitors
EG24713A (en) Methods and systems for marking, tracking and authentication of products
WO2006004884A3 (en) Processes and intermediates useful for preparing fused heterocyclic kinase inhibitors
WO2007076423A3 (en) INHIBITORS OF Akt ACTIVITY
WO2007149523A3 (en) Hexahydro-isoalpha acid based protein kinase modulation cancer treatment
AU2003254053A1 (en) Pyrazolopyrimidines as protein kinase inhibitors
DE60313872D1 (en) PYRAZOLOE1,5-ATPYRIMIDINES AS INHIBITORS CYCLINE-DEPENDENT KINASES
WO2006009765A3 (en) Methods for the identification and use of compounds suitable for the treatment of drug resistant cancer cells
WO2005079300A9 (en) Protein kinase inhibitors and methods for identifying same
WO2005108416A3 (en) Myosin light chain kinase inhibitors and their use
AU2002953255A0 (en) Protein kinase inhibitors
WO2007022042A3 (en) Combinations comrising a protein kinase inhibitor being a pyrimidylaminobξnzamide compound and a hsp90 inhibitor such as 17-aag
WO2005034840A8 (en) Identification of kinase inhibitors
WO2007076320A8 (en) Compounds
WO2007033374A3 (en) Pharmaceutical compositions and methods using temozolomide and a protein kinase inhibitor
WO2005086909A3 (en) Protein kinase c iota
ITPR20020027A1 (en) SPRAYER SPRAYER, IN PARTICULAR FOR AEROSOL THERAPY.
WO2004052919A3 (en) Peptide deformylase inhibitors
AUPS251502A0 (en) Protein kinase inhibitors
WO2007016364A3 (en) Peptide deformylase inhibitors
WO2005005456A3 (en) Peptide deformylase inhibitors
WO2005032550A3 (en) Peptide deformylase inhibitors
WO2002070540A3 (en) Peptide deformylase inhibitors
WO2002070653A3 (en) Peptide deformylase inhibitors
ATE493390T1 (en) 2,3-DIARYL-PYRAZOLIDINE DERIVATIVES AS NEUROTENSIN DEGRADING ENZYME INHIBITORS

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NI NO NZ OM PH PL PT RO RU SC SD SE SG SK SL TJ TM TN TR TT TZ UA UG US UZ VC VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IT LU MC NL PT RO SE SI SK TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
WWE Wipo information: entry into national phase

Ref document number: 2003228345

Country of ref document: AU

WWE Wipo information: entry into national phase

Ref document number: 2478981

Country of ref document: CA

WWE Wipo information: entry into national phase

Ref document number: 2003578895

Country of ref document: JP

WWE Wipo information: entry into national phase

Ref document number: 2003726092

Country of ref document: EP

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
WWP Wipo information: published in national office

Ref document number: 2003726092

Country of ref document: EP